422508-25-6Relevant articles and documents
Microwave-assisted one step synthesis of 8-arylmethyl-9H-purin-6-amines
Tao, Hui,Kang, Yanlong,Taldone, Tony,Chiosis, Gabriela
experimental part, p. 415 - 417 (2011/02/28)
Molecular chaperone heat shock protein 90 (Hsp90) is an important target in cancer and neurodegenerative diseases, and has rapidly become the focus of several drug discovery efforts. Among small molecule Hsp90 inhibitors with clinical applicability are de
Development of a purine-scaffold novel class of hsp90 binders that inhibit the proliferation of cancer cells and induce the degradation of Her2 tyrosine kinase
Chiosis, Gabriela,Lucas, Brian,Shtil, Alexander,Huezo, Henri,Rosen, Neal
, p. 3555 - 3564 (2007/10/03)
The first published synthesis and characterization of a purine-scaffold library of hsp90 inhibitors is presented. The purine-scaffold represents a platform for the creation of easily synthesizable and derivatizable soluble molecules that are amenable for oral administration. The most active compound of the series (71) exhibits binding to hsp90 comparable to the natural product derivative 17AAG that is now in Phase I clinical trial as a cancer therapeutic. 71 Induces the degradation of Her2 tyrosine kinase and arrests the MCF-7 breast cancer cell line at low micromolar concentrations (IC50=2 μM).